Fluorescence imaging can provide valuable information on the expression, distribution, and activity of drug target proteins. Chemical probes are useful small-molecule tools for fluorescence imaging with high structural flexibility and biocompatibility. In this review, we briefly introduce two classes of fluorescent probes for the visualization of drug target proteins. Enzymatically activatable probes make use of the specific enzymatic transformations that generally produce a fluorogenic response upon reacting with target enzymes. Alternatively, specific imaging can be conferred with a ligand that drives the probes to target proteins, where the labeling relies on noncovalent binding, covalent inhibition, or traceless labeling by ligand-directed chemistry.

荧光成像可以提供有关药物靶蛋白表达，分布和活性的有价值的信息。化学探针是有用的小分子工具，用于具有高结构灵活性和生物相容性的荧光成像。在这篇综述中，我们简要介绍了两类用于可视化药物靶蛋白的荧光探针。可酶活化的探针利用通常与靶酶反应后产生荧光应答的特定酶促转化。可选地，可以用驱动探针到达靶蛋白的配体进行特异性成像，其中标记依赖于非共价结合，共价抑制或通过配体定向化学的无痕标记。